Milt Teitler

Summary

Affiliation: Albany Medical College
Country: USA

Publications

  1. ncbi request reprint Ketanserin and spiperone as templates for novel serotonin 5-HT(2A) antagonists
    Richard A Glennon
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
    Curr Top Med Chem 2:539-58. 2002
  2. ncbi request reprint Binding of beta-carbolines at 5-HT(2) serotonin receptors
    Brian Grella
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298 0540, USA
    Bioorg Med Chem Lett 13:4421-5. 2003
  3. ncbi request reprint Determining the oligomer number of native GPCR using florescence correlation spectroscopy and drug-induced inactivation-reactivation
    Milt Teitler
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, New York 12208, USA
    Curr Pharm Biotechnol 15:927-37. 2014
  4. pmc A new approach for studying GPCR dimers: drug-induced inactivation and reactivation to reveal GPCR dimer function in vitro, in primary culture, and in vivo
    Milt Teitler
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
    Pharmacol Ther 133:205-17. 2012
  5. ncbi request reprint Constitutive activity of G-protein coupled receptors: emphasis on serotonin receptors
    Milt Teitler
    Center for Neuroscience and Neuropharmacology, Albany Medical College, 47 New Scotland Avenue, Albany, N Y 12208, USA
    Curr Top Med Chem 2:529-38. 2002
  6. pmc Clozapine and other competitive antagonists reactivate risperidone-inactivated h5-HT7 receptors: radioligand binding and functional evidence for GPCR homodimer protomer interactions
    Milt Teitler
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
    Psychopharmacology (Berl) 212:687-97. 2010
  7. pmc Pharmacological analysis of the novel, rapid, and potent inactivation of the human 5-Hydroxytryptamine7 receptor by risperidone, 9-OH-Risperidone, and other inactivating antagonists
    Jessica A Knight
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208
    Mol Pharmacol 75:374-80. 2009
  8. ncbi request reprint Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs
    Anil Purohit
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
    Psychopharmacology (Berl) 179:461-9. 2005
  9. ncbi request reprint Risperidone irreversibly binds to and inactivates the h5-HT7 serotonin receptor
    Carol Smith
    A 136, Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Ave, Albany, NY 12208, USA
    Mol Pharmacol 70:1264-70. 2006
  10. pmc Risperidone-induced inactivation and clozapine-induced reactivation of rat cortical astrocyte 5-hydroxytryptamine₇ receptors: evidence for in situ G protein-coupled receptor homodimer protomer cross-talk
    Carol Smith
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Ave, Albany, NY 12208, USA
    Mol Pharmacol 79:318-25. 2011

Research Grants

Collaborators

  • Katharine Herrick-Davis
  • Małgorzata Dukat
  • R A Glennon
  • Carol Smith
  • Michael T Klein
  • Anil Purohit
  • Nicole Toohey
  • Jessica A Knight
  • Nantaka Khorana
  • Brian Grella
  • Ashraf A Rahman
  • Jean Chang-Fong
  • Jessica Knight
  • Tariq Rahman
  • Joseph Mazurkiewicz
  • Maha Khalifa Daoud
  • Alberto Malvezzi
  • Antonia Taveres do Amaral
  • Nicholas A Mitchell
  • James Addo

Detail Information

Publications20

  1. ncbi request reprint Ketanserin and spiperone as templates for novel serotonin 5-HT(2A) antagonists
    Richard A Glennon
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
    Curr Top Med Chem 2:539-58. 2002
    ....
  2. ncbi request reprint Binding of beta-carbolines at 5-HT(2) serotonin receptors
    Brian Grella
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298 0540, USA
    Bioorg Med Chem Lett 13:4421-5. 2003
    ..A binding profile was obtained for selected beta-carbolines...
  3. ncbi request reprint Determining the oligomer number of native GPCR using florescence correlation spectroscopy and drug-induced inactivation-reactivation
    Milt Teitler
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, New York 12208, USA
    Curr Pharm Biotechnol 15:927-37. 2014
    ..This approach can be applied to heterodimers as well as homodimers and may aid in the development of novel drugs with heterodimer selectivity. ..
  4. pmc A new approach for studying GPCR dimers: drug-induced inactivation and reactivation to reveal GPCR dimer function in vitro, in primary culture, and in vivo
    Milt Teitler
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
    Pharmacol Ther 133:205-17. 2012
    ..The data obtained using the 5-HT(7) and 5-HT(2A) receptors are strongly supportive of a GPCR homodimer structure, with little evidence of monomer involvement in the function of these receptors...
  5. ncbi request reprint Constitutive activity of G-protein coupled receptors: emphasis on serotonin receptors
    Milt Teitler
    Center for Neuroscience and Neuropharmacology, Albany Medical College, 47 New Scotland Avenue, Albany, N Y 12208, USA
    Curr Top Med Chem 2:529-38. 2002
    ..Studies are presented demonstrating the procedures for producing and characterizing constitutive activated forms of serotonin receptors, including the demonstration of inverse agonist activity of drugs on these receptors...
  6. pmc Clozapine and other competitive antagonists reactivate risperidone-inactivated h5-HT7 receptors: radioligand binding and functional evidence for GPCR homodimer protomer interactions
    Milt Teitler
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
    Psychopharmacology (Berl) 212:687-97. 2010
    ..Although risperidone and 9-OH-risperidone ("inactivating antagonists") completely inactivate the receptor, only 50% of the receptors form a pseudo-irreversible complex with these drugs...
  7. pmc Pharmacological analysis of the novel, rapid, and potent inactivation of the human 5-Hydroxytryptamine7 receptor by risperidone, 9-OH-Risperidone, and other inactivating antagonists
    Jessica A Knight
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208
    Mol Pharmacol 75:374-80. 2009
    ..The rapid, potent inactivation of the receptor-G-protein complex by antagonists implies a constitutive, pre-existing complex between the h5-HT(7) receptor and a G-protein...
  8. ncbi request reprint Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugs
    Anil Purohit
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
    Psychopharmacology (Berl) 179:461-9. 2005
    ..Typical and atypical antipsychotic drugs were assayed for their potencies as inverse agonists at these mutated receptors...
  9. ncbi request reprint Risperidone irreversibly binds to and inactivates the h5-HT7 serotonin receptor
    Carol Smith
    A 136, Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Ave, Albany, NY 12208, USA
    Mol Pharmacol 70:1264-70. 2006
    ..At the very least, the possibility that highly prescribed drugs, such as risperidone, are irreversibly antagonizing GPCR function in vivo is noteworthy...
  10. pmc Risperidone-induced inactivation and clozapine-induced reactivation of rat cortical astrocyte 5-hydroxytryptamine₇ receptors: evidence for in situ G protein-coupled receptor homodimer protomer cross-talk
    Carol Smith
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Ave, Albany, NY 12208, USA
    Mol Pharmacol 79:318-25. 2011
    ..The homodimer structure and protomer-protomer cross-talk offer new avenues of research into receptor dysfunction in disease states and the development of novel drugs...
  11. pmc Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships
    Michael T Klein
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
    J Pharmacol Exp Ther 337:860-7. 2011
    ..The insights generated from this study will inform future drug development and molecular modeling studies for both 5-HT(1E) and 5-HT(1F) receptors...
  12. pmc Human 5-HT7 receptor-induced inactivation of forskolin-stimulated adenylate cyclase by risperidone, 9-OH-risperidone and other "inactivating antagonists"
    Nicole Toohey
    Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
    Mol Pharmacol 76:552-9. 2009
    ..These drugs may produce innovative approaches to the development of therapeutic drugs...
  13. ncbi request reprint Creation, expression, and characterization of a constitutively active mutant of the human serotonin 5-HT6 receptor
    Anil Purohit
    Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, New York 12208, USA
    Synapse 47:218-24. 2003
    ..The inverse agonist action of clozapine indicates that drugs displaying competitive antagonist activity at native 5-HT(6) receptors may display inverse agonist activity at the constitutively activated form of the receptor...
  14. pmc Guinea pig hippocampal 5-HT(1E) receptors: a tool for selective drug development
    Michael T Klein
    Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, New York 12208, USA
    J Neurochem 109:268-74. 2009
    ..Using the guinea pig as an animal model should provide important insights into possible functions of this receptor and the therapeutic potential of selective human 5-HT(1E) drugs...
  15. ncbi request reprint Binding of tetrahydrocarboline derivatives at human 5-HT5A receptors
    Nantaka Khorana
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, Virginia 23298 0540, USA
    J Med Chem 46:3930-7. 2003
    ..Evidence is provided that 5-HT(5A) and 5-HT(2A) receptor affinities probably do not covary and that it might be possible, with continued investigation, to develop analogues with enhanced 5-HT(5A) selectivity...
  16. ncbi request reprint gamma-Carbolines: binding at 5-HT5A serotonin receptors
    Nantaka Khorana
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
    Bioorg Med Chem 11:717-22. 2003
    ..Although 17 also binds at 5-HT(2) receptors, it serves as a novel lead for the further development of 5-HT(5A) ligands...
  17. ncbi request reprint Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG)
    Ashraf A Rahman
    Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, VA 23298 0540, USA
    Bioorg Med Chem Lett 13:1119-23. 2003
    ..38). The quinazoline structure may represent a pharmacologically-active conformation of these agents, and the arylbiguanides were found more lipid soluble than their arylguanidine counterparts at physiological pH...
  18. ncbi request reprint Binding of tryptamine analogs at h5-HT1E receptors: a structure-affinity investigation
    Małgorzata Dukat
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
    Bioorg Med Chem 12:2545-52. 2004
    ..This finding was supported using quantitative structure-activity analysis (QSAR) techniques such as comparative molecular field analysis (CoMFA) and the program QsarIS...
  19. ncbi request reprint Arylguanidine and arylbiguanide binding at 5-HT3 serotonin receptors: a QSAR study
    Richard A Glennon
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
    Bioorg Med Chem 11:4449-54. 2003
    ..A broader examination of 35 arylguanidines and arylbiguanides revealed that affinity could be described by molecular polarizability, a Chi index term (8chiP), and the sum of all (-Cl) E-State values (SsCl) in the molecule...
  20. ncbi request reprint Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptors
    Jean Chang-Fong
    Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
    Bioorg Med Chem Lett 12:155-8. 2002
    ..Detailed re-examination of a compound previously reported to display 100-fold 5-HT(2C) selectivity [i.e., S(+)-5,6-difluoro-alpha-methylisotryptamine] revealed that its selectivity versus 5-HT(2A) receptors was, at best, only 10-fold...

Research Grants2

  1. Molecular Biology of 5HT2A receptor expressing synapses
    Milt Teitler; Fiscal Year: 2005
    ....
  2. Human 5HT 1E Serotonin Receptor Drug Development (RMI)
    Milt Teitler; Fiscal Year: 2005
    ..Selective agonists and antagonists for the 5HT1E receptor should, at the least, provide information on the function of this highly expressed receptor, and may lead to novel therapeutics for brain dysfunction. ..